Antipsychotic Drugs: Classes, Structure-Activity Relationships, and Therapeutic Applications
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Questions and Answers

What are the therapeutic applications of anti-psychotic drugs?

Treatment of psychosis, hallucinations, excitation, and as anti-emetic (D2-blocker)

How do typical antipsychotics act in the body?

Typical antipsychotics act by blocking the action of dopamine D2 receptors

What are the two classifications of symptoms of psychosis?

Positive symptoms (hallucinations and delusions) and Negative symptoms (apathy and social withdrawal)

What are some side effects of anti-psychotic drugs?

<p>Extra-pyramidal symptoms, anti-cholinergic effects, anti-histaminic effects, anti-adrenergic effects, photosensitivity, and retinal toxicity</p> Signup and view all the answers

What is essential for the structure activity relationships of phenothiazine and thioxanthene?

<p>Tricyclic structure, sulfur atom, and electron withdrawing group with an unshared electron at C2</p> Signup and view all the answers

What is the other name for anti-psychotic drugs?

<p>Neuroleptics and Major tranquilizers</p> Signup and view all the answers

What is the most potent substituent at position C2 in phenothiazines and thioxanthenes?

<p>CF3</p> Signup and view all the answers

What is the effect of the absence of a substituent at C2 in phenothiazines and thioxanthenes?

<p>Increased antihistaminic effect and decreased antipsychotic effect</p> Signup and view all the answers

Which substituents interfere with the H-bond formation in phenothiazines and thioxanthenes?

<p>Substituents at C1</p> Signup and view all the answers

What is the effect of substituents at C4 in phenothiazines and thioxanthenes?

<p>Interfere with the sulfur atom receptor binding</p> Signup and view all the answers

What is the essential number of atoms in the chain between N10 and the amino nitrogen for activity in phenothiazines and thioxanthenes?

<p>3</p> Signup and view all the answers

What is the effect of incorporating the amino group into a cyclic structure in phenothiazines and thioxanthenes?

<p>Increases activity</p> Signup and view all the answers

What is the prototype of phenothiazines class, obtained from promethazine?

<p>Chlorpromazine</p> Signup and view all the answers

What is the index that relates the anti-psychotic drug activity to that of Chlorpromazine?

<p>CPZ index</p> Signup and view all the answers

What are the side effects of Chlorpromazine?

<p>Sedation (H1 blocker) &amp; hypotension (α 1-blockage)</p> Signup and view all the answers

What is the advantage of Triflupromazine over Chlorpromazine?

<p>Less sedation &amp; less hypotensive</p> Signup and view all the answers

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